BR112021012242A2 - Esteroides neuroativos de 3-alfa-hidróxi-17-beta-amida e composições destes - Google Patents

Esteroides neuroativos de 3-alfa-hidróxi-17-beta-amida e composições destes Download PDF

Info

Publication number
BR112021012242A2
BR112021012242A2 BR112021012242-7A BR112021012242A BR112021012242A2 BR 112021012242 A2 BR112021012242 A2 BR 112021012242A2 BR 112021012242 A BR112021012242 A BR 112021012242A BR 112021012242 A2 BR112021012242 A2 BR 112021012242A2
Authority
BR
Brazil
Prior art keywords
substituted
unsubstituted
alkyl
compound according
independently hydrogen
Prior art date
Application number
BR112021012242-7A
Other languages
English (en)
Portuguese (pt)
Inventor
Maria Jesus Blanco-Pillado
Francesco G. Salituro
Original Assignee
Sage Therapeutics, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sage Therapeutics, Inc. filed Critical Sage Therapeutics, Inc.
Publication of BR112021012242A2 publication Critical patent/BR112021012242A2/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0011Androstane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J13/00Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/008Ketals at position 17
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified
    • C07J7/007Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified not substituted in position 17 alfa

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
BR112021012242-7A 2018-12-21 2019-12-20 Esteroides neuroativos de 3-alfa-hidróxi-17-beta-amida e composições destes BR112021012242A2 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862784229P 2018-12-21 2018-12-21
US201862784222P 2018-12-21 2018-12-21
US62/784,229 2018-12-21
US62/784,222 2018-12-21
PCT/US2019/067953 WO2020132504A1 (en) 2018-12-21 2019-12-20 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof

Publications (1)

Publication Number Publication Date
BR112021012242A2 true BR112021012242A2 (pt) 2021-09-28

Family

ID=69591712

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021012242-7A BR112021012242A2 (pt) 2018-12-21 2019-12-20 Esteroides neuroativos de 3-alfa-hidróxi-17-beta-amida e composições destes

Country Status (12)

Country Link
US (1) US20220372067A1 (https=)
EP (1) EP3898646B1 (https=)
JP (2) JP7692830B2 (https=)
KR (1) KR20210107050A (https=)
CN (1) CN113195512A (https=)
AU (2) AU2019403415B2 (https=)
BR (1) BR112021012242A2 (https=)
CA (1) CA3124371A1 (https=)
IL (1) IL284183A (https=)
MX (2) MX2021007504A (https=)
TW (2) TWI848034B (https=)
WO (1) WO2020132504A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2806877B2 (en) 2012-01-23 2025-01-29 Sage Therapeutics, Inc. Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
CA2882708A1 (en) 2012-08-21 2014-02-27 Sage Therapeutics, Inc. Methods of treating epilepsy or status epilepticus
KR102396328B1 (ko) 2013-04-17 2022-05-10 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
EP3504189A1 (en) 2016-08-23 2019-07-03 Sage Therapeutics, Inc. A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid
MA51046A (fr) 2017-12-08 2021-03-17 Sage Therapeutics Inc Dérivés de 21-[4-cyano-pyrazol-1-yl]-19-nor-pregan-3. alpha-ol-20-one deutérés pour le traitement de troubles du snc
KR20250174100A (ko) 2018-12-05 2025-12-11 세이지 테라퓨틱스, 인크. 신경활성 스테로이드 및 이의 사용 방법
WO2020132504A1 (en) * 2018-12-21 2020-06-25 Sage Therapeutics, Inc. 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof
US20230250129A1 (en) * 2020-06-24 2023-08-10 Sage Therapeutics, Inc. Neuroactive steroids and compositions thereof
CN119192275B (zh) * 2024-08-22 2025-05-30 湖南玉新药业有限公司 一种3-羰基-4-氮杂-5α-雄甾-17β-羧酸化合物的制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
EP3572417B1 (en) 2011-10-14 2025-12-17 Sage Therapeutics, LLC 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
US9512170B2 (en) * 2013-03-01 2016-12-06 Washington University Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors
CN117024501A (zh) 2014-10-16 2023-11-10 萨奇治疗股份有限公司 靶向cns障碍的组合物和方法
EP4155314A1 (en) 2015-02-20 2023-03-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
KR20250174100A (ko) * 2018-12-05 2025-12-11 세이지 테라퓨틱스, 인크. 신경활성 스테로이드 및 이의 사용 방법
WO2020132504A1 (en) * 2018-12-21 2020-06-25 Sage Therapeutics, Inc. 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof

Also Published As

Publication number Publication date
IL284183A (en) 2021-08-31
TWI892697B (zh) 2025-08-01
AU2019403415B2 (en) 2025-08-21
JP7692830B2 (ja) 2025-06-16
TWI848034B (zh) 2024-07-11
TW202438080A (zh) 2024-10-01
WO2020132504A1 (en) 2020-06-25
EP3898646A1 (en) 2021-10-27
AU2025267433A1 (en) 2025-12-04
CN113195512A (zh) 2021-07-30
AU2019403415A1 (en) 2021-07-08
EP3898646B1 (en) 2026-02-18
CA3124371A1 (en) 2020-06-25
KR20210107050A (ko) 2021-08-31
JP2024107296A (ja) 2024-08-08
MX2021007504A (es) 2021-10-13
US20220372067A1 (en) 2022-11-24
JP2022514385A (ja) 2022-02-10
TW202038967A (zh) 2020-11-01
MX2025000126A (es) 2025-02-10

Similar Documents

Publication Publication Date Title
BR112021012242A2 (pt) Esteroides neuroativos de 3-alfa-hidróxi-17-beta-amida e composições destes
ES2992037T3 (es) Esteroides neuroactivos sustituidos en C7, C12 y C16 y sus procedimientos de utilización
ES2965214T3 (es) Esteroides neuroactivos sustituidos en C17, C20 y C21 y sus procedimientos de utilización
BR112021010996A2 (pt) Esteroides neuroativos e seus métodos de uso
ES2966055T3 (es) Esteroides neuroactivos sustituidos en la posición 10 con un grupo cíclico para su uso en el tratamiento de trastornos del SNC
BR112020012761A2 (pt) composições e métodos para o tratamento de distúrbios do snc
JP2023145726A (ja) CNS障害の処置における使用のためのアザ、オキサ、およびチア-プレグナン-20-オン-3α-オール化合物
BR112017007902B1 (pt) Composto e seu sal, composição farmacêutica e uso do referido composto e seu sal na fabricação de um medicamento para o tratamento de distúrbios do sistema nervoso central
JP2023518411A (ja) 神経刺激性ステロイド及びその使用方法
BR112021007401A2 (pt) esteroides neuroativos insaturados 9(11) e seus métodos de uso
RU2846188C2 (ru) 3альфа-гидрокси-17бета-амидные нейроактивные стероиды и их композиции
BR122024007325A2 (pt) Compostos esteroides neuroativos de 3-alfa-hidróxi-17-beta-amida, suas composições farmacêuticas e seus usos
HK40106568A (en) Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders
BR122024013785A2 (pt) Compostos esteroides neuroativos, composição farmacêutica e seus usos
BR112019000578B1 (pt) Compostos esteróides neuroativos c17, c20 e c21 substituídos, suas composições farmacêuticas e seus usos
BR122022005124B1 (pt) Compostos esteróides neuroativos c17, c20 e c21 substituídos, suas composições farmacêuticas, seus usos e kits
BR122022005119B1 (pt) Compostos esteróides neuroativos c17, c20 e c21 substituídos, suas composições farmacêuticas, seus usos e kits
BR122023013319B1 (pt) Compostos, sal farmaceuticamente aceitável, composição farmacêutica, e usos de um composto

Legal Events

Date Code Title Description
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B154 Notification of filing of divisional application [chapter 15.50 patent gazette]

Free format text: O PEDIDO FOI DIVIDIDO NO BR122024007325-0 PROTOCOLO 870240032499 EM 15/04/2024 17:00.